1.

Generic Name

Phenylephrine, Chlorpheniramine maleate, Sodium citrate, Menthol

2. Qualitative and Quantitative composition

Phenylephrine 5 mg

Chlorpheniramine maleate 2 mg

Sodium citrate 60 mg

Menthol 1 mg

3. Dosage form and strength

Oral syrup containing Phenylephrine 5 mg, Chlorpheniramine maleate 1 mg

4. Clinical particulars
4.1 Therapeutic indication

Sinarest AF Syrup is indicated for treatment of common cold.

4.2 Posology and method of administration

The usual recommended oral dose of Sinarest AF Syrup is:

2-5 years= 2.5ml Three/ Four times a day.

6-12 years= 5ml Three/ Four times a day.

>12 years= 5-10ml Three/ Four times a day.

4.3 Contraindication

The use of Sinarest AF syrup is contraindicated in patients with:

 • Hypersensitivity to any of the ingredients of the formulation.
• Severe hypertension.

4.4 Special warnings and precautions for use

• Caution in elderly patients, hyperthyroidism, myocardial disease, bradycardia, partial
heart block or severe arteriosclerosis when administering phenylephrine.
• Caution in asthma, bladder neck obstruction, cardiovascular disease, COPD, GI
obstruction, glaucoma, hepatic impairment, hyperthyroidism, increased intraocular
pressure, malnutrition, renal impairment, elderly patients, and patients taking CNS
depressants.
• Phenylephrine should be used with care in patients with closed angle glaucoma and
prostatic enlargement.
• Chlorpheniramine, in common with other drugs having anticholinergic effects,
should be used with caution in epilepsy; raised intra-ocular pressure including
glaucoma; prostatic hypertrophy; severe hypertension or cardiovascular disease;
bronchitis, bronchiectasis or asthma; hepatic impairment; renal impairment.
• Children and the elderly are more likely to experience the neurological
anticholinergic effects and paradoxical excitation (eg. increased energy, restlessness,
nervousness). Should not be used with other antihistamine containing products,
including antihistamine containing cough and cold medicines.

4.5 Drug interactions

Phenylephrine: The co-administration of Monoamine Oxidase Inhibitors (MAOIs) or tricyclic

antidepressants and an indirect or mixed-acting sympathomimetic may result in a
hypertensive crisis and hence such concomitant use is best avoided. Additionally
sympathomimetic may reduce the efficacy of beta-blocking and anti-hypertensive drugs.

Not recommended for patients currently receiving or within two weeks of stopping therapy
with monoamine oxidase inhibitors.

Digoxin and cardiac glycosides: concomitant use of phenylephrine may increase the risk of
irregular heartbeat or heart attack.
Chlorpheniramine: Concurrent use of Chlorpheniramine and hypnotics or anxiolytics may
cause an increase in sedative effects; therefore medical advice should be sought before
taking Chlorpheniramine concurrently with these medicines. Chlorpheniramine inhibits
phenytoin metabolism and can lead to phenytoin toxicity. The anti-cholinergic effects of
Chlorpheniramine are intensified by MAOIs.

4.6 Use in special population

• Pediatric: Safe.
• Geriatric: Elderly population may be at greater risk for the side-effects.
• Liver impairment: Use with caution.
• Renal failure: Use with caution.
• Pregnancy and lactation: US Food and Drug Administration (FDA) has specified
Chlorphenamine maleate as a pregnancy category B drug which indicates that animal
and human studies have failed to demonstrate a risk to the fetus in any trimester.
Paracetamol has been specified as a pregnancy category C drug which indicates that
animal studies show an adverse effect on the fetus but there are no teratogenic
studies of Paracetamol in pregnant women. Sinarest is recommended to be taken
during pregnancy only under doctor's recommendation.

4.7 Effects on ability to drive and use machine

It is advisable not to drive or operate machinery when on treatment with Sinarest AF syrup.

4.8 Undesirable effects

Sinarest AF syrup is generally well tolerated and adverse events are rare. Anaphylactic
reaction ,Thrombocytopenia, Palpitations, Tachycardia, Bradycardia, Tinnitus, Vertigo,
Periorbital oedema, Vision blurred , Periorbital swelling, Eye swelling, Conjunctivitis,
Nausea, Vomiting Diarrhoea, Dry mouth, Dyspepsia, Constipation, Abdominal pain, Hepatic
function abnormal , Decreased appetite, Back pain, Myalgia, Dysuria, Urinary retention,
Dyspnoea, Rash, Pruritus , Urticaria, Angioedema, Diabetes insipidus, Metabolic acidosis,
Lactic acidosis, Headache, Dizziness.

4.9 Overdose
There is limited experience of overdose with Sinarest AF syrup. Initiate general symptomatic
and supportive measures in all cases of overdosages where necessary.

5. Pharmacological properties
5.1 Mechanism of action

Phenylephrine decreases nasal congestion by acting on α1-adrenergic receptors in the

arterioles of the nasal mucosa to produce constriction; this leads to decreased edema and
increased drainage of the sinus cavities.

In allergic reactions an allergen interacts with and cross-links surface IgE antibodies on mast
cells and basophils. Once the mast cell-antibody-antigen complex is formed, a complex
series of events occurs that eventually leads to cell-degranulation and the release of
histamine (and other chemical mediators) from the mast cell or basophil. Once released,
histamine can react with local or widespread tissues through histamine receptors.
Histamine, acting on H1-receptors, produces pruritis, vasodilatation, hypotension, flushing,
headache, tachycardia, and bronchoconstriction. Histamine also increases vascular
permeability and potentiates pain. Chlorpheniramine maleate binds to the histamine H1
receptor. This block the action of endogenous histamine, which subsequently leads to
temporary relief of the negative symptoms brought on by histamine.

The Sodium citrate in Sinarest AF Syrup liquefies mucus and helps expectoration.

Menthol has a cooling and soothing effect.

5.2 Pharmacodynamic properties

Phenylephrine is a powerful vasoconstrictor. It is used as a nasal decongestant and

cardiotonic agent. Phenylephrine is a postsynaptic α1-receptor agonist with little effect on
β-receptors of the heart. Parentral administration of Phenylephrine causes a rise in systolic
and diastolic pressures, a slight decrease in cardiac output, and a considerable increase in
peripheral resistance; most vascular beds are constricted, and renal, splanchnic, cutaneous,
and limb blood flows are reduced while coronary blood flow is increased. Phenylephrine
also causes pulmonary vessel constriction and subsequent increase in pulmonary arterial
pressure. Vasoconstriction in the mucosa of the respiratory tract leads to decreased edema
and increased drainage of sinus cavities.

Chlorpheniramine maleate is a histamine H1 antagonist of the alkylamine class. It competes

with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal
tract, blood vessels and respiratory tract. It provides effective, temporary relief of sneezing,
watery and itchy eyes, and runny nose due to hay fever and other upper respiratory
allergies.

Citrate prevents activation of the clotting cascade by chelating calcium ions. Citrate
neutralizes acid in the stomach and urine, raising the pH.

5.3 Pharmacokinetic properties

Phenylephrine has low oral bioavailability owing to irregular absorption and first-pass
metabolism by monoamine oxidase in the gut and liver. When injected subcutaneously or
intramuscularly it takes 10 to 15 minutes to act; subcutaneous and intramuscular injections
are effective for up to about 1 hour and up to about 2 hours, respectively. Intravenous
injections are effective for about 20 minutes. Systemic absorption follows topical
application.

Chlorphenamine maleate is absorbed relatively slowly from the gastrointestinal tract, peak
plasma concentrations occurring about 2.5 to 6 hours after oral doses. Bioavailability is low,
values of 25 to 50% having been reported. Chlorphenamine appears to undergo
considerable first-pass metabolism. About 70% of Chlorphenamine in the circulation is
bound to plasma proteins. There is wide inter individual variation in the pharmacokinetics of
Chlorphenamine; values ranging from 2 to 43 hours have been reported for the half-life.
Chlorphenamine is widely distributed in the body, and enters the CNS. Chlorphenamine
maleate is extensively metabolised. Metabolites include desmethyl- and
didesmethylchlorphenamine. Unchanged drug and metabolites are excreted primarily in the
urine; excretion is dependent on urinary pH and flow rate. Only trace amounts have been
found in the faeces. Duration of action of 4 to 6 hours has been reported; this is shorter
than may be predicted from pharmacokinetic parameters. More rapid and extensive
absorption, faster clearance, and a shorter half-life have been reported in children.
Sodium citrate is metabolised after absorption to bicarbonate. Bicarbonate ions are
excreted in the urine, which is rendered alkaline, and there is an accompanying diuresis.

6. Nonclinical properties
6.1 Animal Toxicology or Pharmacology

NA.

7. Description

Phenylephrine is in a class of medications called nasal decongestants. Its chemical name is

hydrogen 3-[(1R)-1-hydroxy-2-(methylamino)ethyl] phenol chloride and its structural
formula is:

Its empirical formula is C9H13NO2, and its molecular weight is 167.2 g/mol.

Chlorpheniramine maleate is in a class of medications called antihistamines. Its chemical

name is(2Z)-but-2-enedioic acid; [3-(4-chlorophenyl)-3-(pyridin-2-yl)propyl] dimethylamine
and its structural formula is :

Its empirical formula is C16H19ClN2.C4H4O4 or C20H23ClN2O4and its molecular weight is 390.9.

8. Pharmaceutical particulars
8.1 Incompatibilities
There are no known incompatibilities.

8.2 Shelf-life

36 months.

8.3 Packaging Information

Sinarest AF syrup is available in bottles of 60 ml.

8.4 Storage and handling instructions

Store below 30 ⁰C in a dark and dry place.

9. Patient Counselling Information

9.1 Adverse Reactions

Refer part 4.8

9.2 Drug Interactions

Refer part 4.5

9.3 Dosage

Refer part 4.2

9.4 Storage

Refer part 8.4

9.5 Risk Factors

Refer part 4.4

9.6 Self-monitoring information

NA
 9.7 Information on when to contact a health care provider or seek emergency
help

Patient is advised to be alert for the emergence or worsening of the adverse reactions and
contact the prescribing physician.

9.8 Contraindications

Refer part 4.3

10. Manufactured by

CENTAUR PHARMACEUTICALS PVT. LTD.

11. Details of permission or license number with date

158(249)/MFG/DFDA/2013/5447 dated. 01.03.2013 for domestic.

12. Date of revision: January 2022